Posted by Chairman_MAO on September 27, 2005, at 21:51:32
In reply to Triple Reuptake Inhibitors - Race to Market, posted by jrbecker on September 27, 2005, at 8:20:32
If you take tranylcypromine at 120mg/day or more, you are taking a triple uptake inhibitor:
para-Hydroxytranylcypromine (p-OHTCP) has recently been unequivocally identified in our laboratory as a metabolite of the antidepressant tranylcypromine (TCP). In the study reported here, we have determined brain and heart levels of p-OHTCP in the rat after intraperitoneal administration of a 0.1 mmol/kg dose of TCP or N-(2-cyanoethyl)tranylcypromine (CE-TCP). The animals were killed at 5, 15, 30, 60, 120 or 240 min after drug administration and the tissues (brain and heart) rapidly dissected out. The tissues were frozen in isopentane on solid carbon dioxide and stored at -20 degrees C until time of analysis. Tissue levels of p-OHTCP, TCP and CE-TCP were determined after aqueous pentafluorobenzoylation by conducting analyses with a gas-liquid chromatograph equipped with a fused silica (SE-54) capillary column and an electron-capture detector. Our results show that substantial concentrations of p-OHTCP were present in both brain and heart after TCP and CE-TCP administration. Higher levels of p-OHTCP were present in the brain than in the heart after TCP treatment, but this situation was reversed with the CE-TCP-treated rats. Since p-OHTCP has been shown to retain some MAO-inhibiting properties and to have effects on uptake of catecholamines and serotonin it could therefore contribute to the pharmacological profile of TCP.
I wish they'd throw that drug in a patch, man. ;)
BTW: My doctor switched me back to tranylcypromine 120mg/day + Lunesta because I just couldnt take phenelzine anymore (complete inability to have sex). At least I have a hip enough doctor that he doesnt have a problem with giving me 12 tabs per day. Too bad my lunesta script is only 1mg, but he said we can titrate up. I just want to sleep!
What would be really cool is if I had enough sedation to allow me to take the TCP at bedtime. Then I could maintain steady state plasma levels at all times of the metabolitse. rockin'
P.S. My phenylethylidenehydrazine synth is coming along. We need some input tho: the freebase cannot survive the stomach and is an oil. Making a decent salt is hard. any other ideas?
poster:Chairman_MAO
thread:560146
URL: http://www.dr-bob.org/babble/20050927/msgs/560408.html